نتایج جستجو برای: acetylcholinesterase inhibitor

تعداد نتایج: 217751  

2014
Shana V. Stoddard Mark T. Hamann Randy M. Wadkins

Due to the diversity of biological activities that can be found in aquatic ecosystems, marine metabolites have been an active area of drug discovery for the last 30 years. Marine metabolites have been found to inhibit a number of enzymes important in the treatment of human disease. Here, we focus on marine metabolites that inhibit the enzyme acetylcholinesterase, which is the cellular target fo...

Journal: :Molecules 2010
Jan Korabecny Kamil Musilek Ondrej Holas Eugenie Nepovimova Daniel Jun Filip Zemek Veronika Opletalova Jiri Patocka Vlastimil Dohnal Florian Nachon Jana Hroudova Zdenek Fisar Kamil Kuca

A new tacrine based cholinesterase inhibitor, N-(bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine (1), was designed and synthesized to interact with specific regions of human acetylcholinesterase and human butyrylcholinesterase. Its inhibitory ability towards cholinesterases was determined and compared to tacrine (THA) and 9-amino-7-methoxy-1,2,3,4-tetrahydroacridine (7-MEOTA). T...

2010
Jong-Kug Lee Jeong-Hoon Jang Jong-Tae Lee Jong-Soo Lee

To develop a potent anti-obesity lipase inhibitor from mushroom, the lipase inhibitory activities of various mushroom extracts were determined. Methanol extracts from Phellinus linteus fruiting body exhibited the highest lipase inhibitory activity (72.8%). The inhibitor was maximally extracted by treatment of a P. linteus fruiting body with 80% methanol at 40℃ for 24 hr. After partial purificat...

Journal: :Biochemistry 2002
P Bar-On C B Millard M Harel H Dvir A Enz J L Sussman I Silman

Rivastigmine, a carbamate inhibitor of acetylcholinesterase, is already in use for treatment of Alzheimer's disease under the trade name of Exelon. Rivastigmine carbamylates Torpedo californica acetylcholinesterase very slowly (k(i) = 2.0 M(-1) min(-1)), whereas the bimolecular rate constant for inhibition of human acetylcholinesterase is >1600-fold higher (k(i) = 3300 M(-1) min(-1)). For human...

Journal: :Acta poloniae pharmaceutica 2009
Marek Bajda Anna Wieckowska Barbara Malawska

An electrophoretically mediated microanalysis technique was developed for the rapid screening of acetylcholinesterase inhibitors. Activity of four original compounds, N-benzylpiperidine, carbamoyloxyphenyl derivatives and reference inhibitor--tacrine was determined and compared with the data obtained from Ellman's assay. Percentage of enzyme inhibition detected at inhibitor concentration of 3.3...

Journal: :journal of physical & theoretical chemistry 2015
leila pishkar parisa r. jamaat somayeh makarem

tacrine (9-amino-1,2,3,4-tetrahydroacridine) as a reversible inhibitor of acetylcholinesterase (ache),was the first drug for the symptomatic treatment of alzheimer’s disease (ad). nmr structuredetermination still presents some considerable challenges: the method is limited to systems ofrelatively small molecular mass, data collection times are long, data analysis remains a lengthyprocedure, and...

2002
Hong Zhu Ing K. Ho Robert E. Kramer Rodney C. Baker

The cholinergic system has been proposed to participate in the development of dependence on opioids. The present study examined effects of dermal pretreatment with methyl parathion (MP), an acetylcholinesterase inhibitor, on the development of physical dependence on morphine. Opioid dependence was induced by continuous intracerebroventricular (i.c.v.) infusion of morphine (26 nmol/μl/h) for 3 d...

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